| Size | Price | |
|---|---|---|
| Other Sizes |
| ln Vitro |
Treatment with pargyline (0.5-2 mM; 24-120 hours; LNCaP-LN3 cells) inhibits prostate cancer cell proliferation in a dose- and time-dependent manner [2]. In a dose-dependent manner, pargyline (0.5-2 mM; 24-48 hours; LNCaP-LN3 cells) treatment decreases the S phase and increases the G1 phase in cells [2]. Treatment of LNCaP-LN3 cells with 0.5 mM of pargyline for 24 hours increases apoptosis [2]. Treatment with pargyline (2 mM; 48 hours; LNCaP-LN3 cells) causes a rise in cytochrome c and a fall in caspase-3 in cells, but it has no effect on BCL-2 expression [2].
|
|---|---|
| ln Vivo |
When pargyline (10 mg/kg; intravenously) is administered to unanesthetized adult spontaneously hypertensive rats (SHR) in normotensive rats, the treatment causes a moderate (about 20 mm Hg) but long-lasting (48 h) drop in systolic blood pressure. Alternatively [3]. Arterial pressure decreases when 200 μg of icv pargyline is injected directly into the brain. The build-up of norepinephrine at inhibitory α-adrenergic receptors in the brain appears to be the cause of pargylline's hypotensive impact in SHR [3].
|
| Cell Assay |
Cell Proliferation Assay[2]
Cell Types: LNCaP-LN3 Cell Tested Concentrations: 0.5 mM, 1 mM, 1.5 mM or 2 mM Incubation Duration: 24 hrs (hours), 48 hrs (hours), 72 hrs (hours), 96 hrs (hours) or 120 hrs (hours) Experimental Results: Inhibition of proliferation of prostate cancer cells in a time- and dose-dependent manner. Cell cycle analysis [2] Cell Types: LNCaP-LN3 Cell Tested Concentrations: 0.5 mM, 2 mM Incubation Duration: 24 hrs (hours), 48 hrs (hours) Experimental Results: The proportion of cells in S phase diminished and the proportion of G1 phase increased. Apoptosis analysis[2] Cell Types: LNCaP-LN3 Cell Tested Concentrations: 0.5 mM Incubation Duration: 24 hrs (hours) Experimental Results: Increased apoptotic cells. Western Blot Analysis[2] Cell Types: LNCaP-LN3 Cell Tested Concentrations: 2 mM Incubation Duration: 48 hrs (hours) Experimental Results: Induction of increased cytochrome c and diminished caspase-3. |
| References |
|
| Additional Infomation |
Pargyline is an aromatic amine.
Pargyline is a monoamine oxidase inhibitor with antihypertensive properties. Pargyline is a monoamine oxidase (MAO) inhibitor with antidepressant activity. Pargyline selectively inhibits MAO type B, an enzyme catalyzing the oxidative deamination and inactivation of certain catecholamines, such as norepinephrine and dopamine, within the presynaptic nerve terminals. By inhibiting the metabolism of these biogenic amines in the brain, pargyline increases their concentration and binding to postsynaptic receptors. Increased receptor stimulation may cause downregulation of central receptors which may attribute to pargyline's antidepressant effect. A monoamine oxidase inhibitor with antihypertensive properties. See also: Methyclothiazide; pargyline hydrochloride (annotation moved to). Drug Indication For the treatment of moderate to severe hypertension. Mechanism of Action MAOIs act by inhibiting the activity of monoamine oxidase, thus preventing the breakdown of monoamine neurotransmitters and thereby increasing their availability. There are two isoforms of monoamine oxidase, MAO-A and MAO-B. MAO-A preferentially deaminates serotonin, melatonin, epinephrine and norepinephrine. MAO-B preferentially deaminates phenylethylamine and trace amines. Pargyline functions by inhibiting the metabolism of catecholamines and tyramine within presynaptic nerve terminals. Catecholamines cause general physiological changes that prepare the body for physical activity (fight-or-flight response). Some typical effects are increases in heart rate, blood pressure, blood glucose levels, and a general reaction of the sympathetic nervous system. |
| Molecular Formula |
C11H13N
|
|---|---|
| Molecular Weight |
159.23
|
| Exact Mass |
159.105
|
| CAS # |
555-57-7
|
| Related CAS # |
Pargyline hydrochloride;306-07-0
|
| PubChem CID |
4688
|
| Appearance |
Colorless to light yellow liquid
|
| Density |
0.94
|
| Boiling Point |
86-88ºC(4 torr)
|
| Melting Point |
156 - 160ºC
|
| Flash Point |
83ºC
|
| Index of Refraction |
n20/D 1.522(lit.)
|
| LogP |
1.751
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
1
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
12
|
| Complexity |
159
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
N(C([H])([H])[H])(C([H])([H])C#C[H])C([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H]
|
| InChi Key |
DPWPWRLQFGFJFI-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C11H13N/c1-3-9-12(2)10-11-7-5-4-6-8-11/h1,4-8H,9-10H2,2H3
|
| Chemical Name |
N-benzyl-N-methylprop-2-yn-1-amine
|
| Synonyms |
Eudatin; Pargyline
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~628.02 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (15.70 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (15.70 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (15.70 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 6.2802 mL | 31.4011 mL | 62.8022 mL | |
| 5 mM | 1.2560 mL | 6.2802 mL | 12.5604 mL | |
| 10 mM | 0.6280 mL | 3.1401 mL | 6.2802 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
